Konzeptionell neu ist die Synthese von 2‐Aminoindolen durch Palladium‐katalysierte Reaktion von N‐Alkinylaniliden mit primären oder sekundären Aminen (siehe Schema). Ihr Schlüsselschritt ist die Bildung eines σ,π‐gebundenen Palladacyclus, an dessen aktivierte Alkineinheit ein externes Stickstoffnucleophil unter Aufbau des Indolgerüsts addiert. (X=I, Br; HNR2R3=primäres oder sekundäres Amin; Ts=Tosyl.)
Indole derivatives
Indole derivatives R 0140Palladium-Catalyzed Synthesis of 2-Aminoindoles by a Heteroannulation Reaction. -The synthesis of 2-substituted indoles is based on a novel palladium-catalyzed cross-coupling sequence between N-alkynyl-2-halogenanilides and primary as well as secondary amines. Adding potassium carbonate to the reaction mixture reduces the required excess of amines. -(WITULSKI*, B.; ALAYRAC, C.; TEVZADZE-SAEFTEL, L.; Angew.
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